C-82

C-82 is a β-catenin/CREB-binding protein (CBP) inhibitor and an active metabolite of PRI-724 (Item No. 41728).¹ It reduces the proliferation and protein levels of cyclin D1, α-smooth muscle actin (α-Sma), and Ki-67, a marker of cell proliferation, in primary mouse hepatic stellate cells (HSCs) when used at a concentration of 10 µM. C-82 (10 µM) decreases viability in continuous culture-activated primary mouse HSCs. It induces apoptosis when used in combination with nilotinib (Item Nos. 10010422 | 36628) in non-stem- and stem cell subpopulations of tyrosine kinase inhibitor-resistant, patient-derived, and blast crisis phase chronic myeloid leukemia (CML) cells with or without co-culture of primary human bone marrow mesenchymal stromal cells (MSCs).²

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1. Osawa, Y., Oboki, K., Imamura, J., et al. Inhibition of cyclic adenosine monophosphate (cAMP)-response element-binding protein (CREB)-binding protein (CBP)/β-catenin reduces liver fibrosis in mice. EBioMedicine 2(11), 1751-1758 (2015).

2. Zhou, H., Mak, P.Y., Mu, H., et al. Combined inhibition of β-catenin and Bcr-Abl synergistically targets tyrosine kinase inhibitor-resistant blast crisis chronic myeloid leukemia blasts and progenitors in vitro and in vivo. Leukemia 31(10), 2065-2074 (2017).